合成路线:By reaction of thienamycin (I) with methyl formimidate (II) by means of NaOH in water.
参考文献标题:MK-0787
文献作者:Serradell,M.N.; Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1980,5(3),136
合成路线:The reaction of (3R,5R,6S)-6-(1(R)-hydroxyethyl)-2-oxo-1-carbapenem-3-carboxylic acid p-nitrobenzyl ester (I) with diphenyl chlorophosphate by (II) means of DMAP and DIEA in DMA/dichloromethane gives the enol phosphate (III),which is condensed with 2-aminoethanethiol (IV) in DMA to yield the 2-aminoethylsulfanyl derivative (V).The reaction of (V) with benzyl formimidate (VI) by means of DIEA in DMA affords the intermediate p-nitrobenzyl ester (VII),which is finally hydrogenated with H2 over Pd/C in water/isopropanol/N-methylmorpholine to provide the target Imipemide.
参考文献标题:Process for the preparation of imipenem
文献作者:Kumar,Y.; Tewari,N.; Rai,B.P.(Ranbaxy Laboratories Ltd.)
参考来源:WO 0294828
合成路线:The condensation of 7-oxo-6-(1-hydroxyethyl)-3-(diphenoxyphosphate)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid p-nitrophenyl ester (I) with the bis(trimethylsilyl) derivative of 2-(iminomethylamino)ethanethiol (II) in the presence of base gives p-nitrophenyl ester of MK-0787,protected with a trimethylsilyl group (III),which is finally deprotected by hydrogenolysis.
参考文献标题:A direct transformation of bicyclic keto esters to N-formimidoyl thienamycin
文献作者:Reamer,R.a.; Sletzinger,M.; Hartner,F.W.; Liu,T.; Shinkai,I.
参考来源:Tetrahedron Lett 1982,23(47),4903
产品链接: CAS No. 74431-23-5›› 产品链接: CAS No.64221-86-9››